Bigelovin 是可从朝阳花中分离得到的一种倍半萜内酯，是选择性的视黄素 X 受体 α (retinoid X receptor α) 的激动剂。Bigelovin 可通过诱导凋亡和自噬来发挥抗肿瘤活性。Bigelovin 通过抑制ROS的生成来调节 mTOR 信号通路。
| 生物活性 | Bigelovin, a sesquiterpene lactone isolated fromInula hupehensis, is a selectiveretinoid X receptor αagonist. Bigelovin suppresses tumor growth through inducingapoptosisandautophagyvia the inhibition ofmTORpathway regulated by ROS generation[1]. |
体外研究
(In Vitro) | Bigelovin (0-20 μM, 24-72 h) significantly inhibits cell viability of liver cancer cells and induces apoptosis and autophagy[1].
Bigelovin causes a significant increase of p62, LC3B-II, Beclin-1 and a corresponding decrease of p62 levels in a time-dependent manner[1].
Bigelovin induces cell death involves the suppression of mTOR pathway regulated by ROS production[1].
Cell Viability Assay[1] | Cell Line: | HepG2 and SMMC-7721 cells. | | Concentration: | 0-20 μM. | | Incubation Time: | 24, 48, 72 h. | | Result: | Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time
dependent manner.
No significant difference observed in cell viability of normal liver cell lines, LO2 and
LX2, after BigV treatment for 24, 48 or 72 h.
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Western Blot Analysis[1] | Cell Line: | HepG2 and SMMC-7721 cells. | | Concentration: | 0-10 μM. | | Incubation Time: | 24 h. | | Result: | The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment.
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体内研究
(In Vivo) | Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model[1].
| Animal Model: | HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1]. | | Dosage: | 5, 10, 20 mg/kg. | | Administration: | Intravenous injection every 2 days. | | Result: | The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight.
No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration.
Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII
levels.
The inactivation of mTOR was also observed in tumor tissues
isolated from BigV-treated mice.
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| Formula | |
| CAS 号 | |
| 结构分类 | - Ketones, Aldehydes, Acids
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| 来源 | - Plants
- Compositae
- Inula hupehensis
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(328.58 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2858 mL | 16.4290 mL | 32.8580 mL | | 5 mM | 0.6572 mL | 3.2858 mL | 6.5716 mL | | 10 mM | 0.3286 mL | 1.6429 mL | 3.2858 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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